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GENITO URINARY SYSTEM AND SEX HORMONES › SEX HORMONES AND MODULATORS OF THE GENITAL SYSTEM › HORMONAL CONTRACEPTIVES FOR SYSTEMIC USE › Progestogens and estrogens, sequential preparations
levonorgestrel and ethinylestradiol
G03AB03
Forms & Strengths
- Oral tablets: Levonorgestrel 0.1 mg / Ethinyl estradiol 0.02 mg
- Oral tablets: Levonorgestrel 0.15 mg / Ethinyl estradiol 0.03 mg
- Multiphasic oral tablets: Various regimens (e.g., 0.05/0.03 mg, 0.075/0.04 mg, 0.125/0.03 mg)
Adult Dosing
- Contraception: 1 tablet daily taken orally at the same time each day for 21 or 24 active days, followed by 7 or 4 inactive/hormone-free days or continued active pills for extended regimens
- Missed dose: If 1 active pill is missed, take as soon as remembered and continue daily dosing; if 2 or more active pills are missed, take the most recent missed pill and use backup contraception for 7 days
Pediatric Dosing
- Postmenarchal adolescents: 1 tablet daily as outlined in the adult regimen for contraception
Indications
- Prevention of pregnancy
- Management of moderate acne vulgaris in females aged 15 and older (specific formulations)
- Treatment of symptoms of premenstrual dysphoric disorder (PMDD) in females choosing oral contraception
Mechanism of Action
- Suppression of gonadotropins (LH and FSH) via negative feedback on the hypothalamus and pituitary
- Inhibition of ovulation
- Alteration of cervical mucus to impede sperm penetration
- Atrophy of the endometrium to prevent implantation
Contraindications
- Known or suspected pregnancy
- History of thrombophlebitis or thromboembolic disorders (DVT, PE)
- Active or past history of cerebrovascular disease or coronary artery disease
- Valvular heart disease with thrombogenic complications
- Known or suspected carcinoma of the breast or estrogen-sensitive neoplasms
- Undiagnosed abnormal uterine bleeding
- Hepatic tumor, severe hepatic disease, or impaired liver function
- Hypersensitivity to any component of the product
- Smoking in women over 35 years of age
Adverse Reactions
- Common: Nausea, abdominal cramping, breakthrough bleeding, spotting, amenorrhea, breast tenderness
- Common: Headache, migraine, mood changes, weight fluctuation, fluid retention
- Serious: Venous and arterial thromboembolism (DVT, pulmonary embolism, myocardial infarction, stroke)
- Serious: Hypertension, hepatic adenomas, gallbladder disease, hypertriglyceridemia
Drug Interactions
- CYP3A4 inducers (e.g., rifampin, barbiturates, carbamazepine, St. John's wort) decrease contraceptive efficacy
- CYP3A4 inhibitors (e.g., ketoconazole, fluconazole, grapefruit juice) may increase plasma concentrations of ethinyl estradiol
- Anticonvulsants (e.g., lamotrigine) may experience reduced therapeutic efficacy when co-administered with estrogen-containing contraceptives
- Antidiabetic agents: Hormonal contraceptives may decrease glucose tolerance, requiring dosage adjustments of insulin or oral hypoglycemics
Curated Content: Needs Vetting Before Put to Clinical Use